Abstract
Pomegranate (Punica granatum) seed linolenic acid isomers were evaluated as selective estrogen receptor modulators (SERMs) in vitro. Punicic acid (PA) inhibited (IC(50)) estrogen receptor (ER) alpha at 7.2 microM, ERbeta at 8.8 microM; alpha-eleostearic acid (AEA) inhibited ERalpha/ERbeta at 6.5/7.8 microM. PA (not AEA) agonized ERalpha/ERbeta (EC(50)) at 1.8/2 microM, antagonizing at 101/80 microM. AEA antagonized ERalpha/ERbeta at 150/140 microM. PA and AEA induced ERalpha and ERbeta mRNA expression in MCF-7, but not in MDA-MB-231. Overall, the results show PA and AEA are SERMs.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Breast Neoplasms
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Cell Division / drug effects
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Cell Line, Tumor
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Dose-Response Relationship, Drug
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Estrogen Receptor alpha / genetics
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Estrogen Receptor alpha / metabolism
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Estrogen Receptor beta / genetics
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Estrogen Receptor beta / metabolism
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Fatty Acids / analysis
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Humans
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Isomerism
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Linoleic Acids / chemistry
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Linoleic Acids / metabolism
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Linoleic Acids / pharmacology*
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Linoleic Acids, Conjugated / metabolism
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Linolenic Acids / metabolism
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Lythraceae / chemistry*
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Phytoestrogens / metabolism
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Phytoestrogens / pharmacology*
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Plant Oils / chemistry
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RNA, Messenger / analysis
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Receptors, Estrogen / drug effects*
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Receptors, Estrogen / physiology*
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Reverse Transcriptase Polymerase Chain Reaction
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Seeds / chemistry*
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Selective Estrogen Receptor Modulators / metabolism
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Selective Estrogen Receptor Modulators / pharmacology
Substances
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Estrogen Receptor alpha
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Estrogen Receptor beta
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Fatty Acids
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Linoleic Acids
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Linoleic Acids, Conjugated
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Linolenic Acids
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Phytoestrogens
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Plant Oils
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RNA, Messenger
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Receptors, Estrogen
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Selective Estrogen Receptor Modulators